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Assay Detail

CHEMBL872600

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Compound was tested in vitro for its ability to inhibit serine protease thrombin using succinyl-Ala-p-nitroanilide as substrate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.
Lu T, Tomczuk B, Illig CR, Bone R, Murphy L, Spurlino J, Salemme FR, Soll RM.
Bioorg Med Chem Lett (1998) 8 : 1595 -1600
PubMed 9873397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.42 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41876 1 8.34
CHEMBL289951 1 7.96
CHEMBL287807 1 7.89
CHEMBL291062 1 7.48
CHEMBL282549 1 7.16
CHEMBL287910 1 6.58
CHEMBL41862 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41876 Ki = 4.6 nM 8.34
CHEMBL289951 Ki = 11.0 nM 7.96
CHEMBL287807 Ki = 13.0 nM 7.89
CHEMBL291062 Ki = 33.0 nM 7.48
CHEMBL282549 Ki = 70.0 nM 7.16
CHEMBL287910 Ki = 260.0 nM 6.58
CHEMBL41862 Ki = 320.0 nM 6.50